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. 2008 May 6;13(5-2):454–463. doi: 10.1016/j.ccr.2008.03.004

Table 1.

Tenovin SAR Studies Aimed at Increasing Water Solubility

ID Inline graphic
p53 Increasea K40Ac Tubulin Increaseb SirT2 Inhibitionc
R1 R2
Tenovin-1 tBu NHCOCH3 + + +
Tenovin-2 tBu NHCOCH(CH3)2 + + +
Tenovin-3 tBu NH2 + + +
Tenovin-4 N3 NHCOCH3
Tenovin-5 tBu NHCOPh + + +
Tenovin-6 tBu NHCO(CH2)4NMe2.HCl + + +
a

Ability to increase p53 levels was determined in MCF-7 cells treated for 6 hr at 10 μM as described in Figure 1B.

b

Ability to increase K40 Ac-tubulin levels was determined in H1299 cells treated as described in Figure 7B.

c

SirT2 inhibition assessed as described in Figure 5B using a compound concentration of 10 or 30 μM depending on the compound's solubility in the assay buffer.